Day: February 23, 2023

Association between health-related quality of life and symptoms in patients with chronic constipation: an integrated analysis of three phase 3 trials of prucalopride was written by Tack, J.;Camilleri, M.;Dubois, D.;Vandeplassche, L.;Joseph, A.;Kerstens, R.. And the article was included in Neurogastroenterology & Motility in 2015.Quality Control of 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide This article mentions the following:

Background : Prucalopride is a high-affinity 5-HT₄ receptor agonist for the treatment of chronic constipation. The aims of this study were to investigate the relationship between health-related quality of life (HRQoL) and symptoms of constipation, and to assess the response of HRQoL to treatment using integrated data from three phase III trials of prucalopride. Methods : This was an integrated anal. of data from three pivotal multicenter, double-blind, randomized, placebo-controlled, parallel-group trials (ClinicalTrials.gov Identifiers: NCT00488137, NCT00483886 and NCT00485940). Relationships were investigated between Patient Assessment of Constipation Quality of Life (PAC-QOL) scores, Patient Assessment of Constipation Symptoms (PAC-SYM) scores, bowel movement frequency (assessed using daily diaries), and treatment. Key Results : Patients treated with prucalopride 2 mg (n = 659) and placebo (n = 661) were included in the anal. An improvement in PAC-SYM scores correlated well with an improvement in PAC-QOL overall score (r = 0.711) and satisfaction subscale score (r = 0.589). After 12 wk, PAC-QOL overall score and satisfaction subscale score significantly (p < 0.001) improved by ≥1 point (clin. relevant) in 36.5% and 44.1% of patients treated with prucalopride, compared with 18.5% and 22.4% with placebo resp. Moreover, 39.0% of patients with an improvement in satisfaction of ≥1 point achieved ≥3 spontaneous complete bowel movements/wk, compared with 7.4% of those with no improvement in satisfaction (<1 point). Conclusions & Inferences : Improvements in PAC-QOL overall score and satisfaction score were associated with improvements in symptoms of chronic constipation. Compared with placebo, treatment with prucalopride significantly improved HRQoL. In the experiment, the researchers used many compounds, for example, 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide (cas: 179474-81-8Quality Control of 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide).

4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide (cas: 179474-81-8) belongs to benzofurans derivatives. Benzofuran is the “”parent”” of many related compounds with more complex structures. For example, psoralen is a benzofuran derivative that occurs in several plants. Substituted benzofurans find applications such as fluorescent sensors, oxidants, in drug discovery, and in another field of chemistry and agriculture.Quality Control of 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

PIM kinase-responsive microsecond-lifetime photoluminescent probes based on selenium-containing heteroaromatic tricycle was written by Ekambaram, Ramesh;Babu Manoharan, Ganesh;Enkvist, Erki;Ligi, Kadri;Knapp, Stefan;Uri, Asko. And the article was included in RSC Advances in 2015.Product Details of 330555-71-0 This article mentions the following:

A new structural fragment was synthesized for construction of protein binding-responsive photoluminescent probes. In complex with protein kinases of the PIM family, bisubstrate inhibitors containing benzo[4,5]seleno[3,2-d]pyrimidin-4-one moiety revealed microsecond-lifetime phosphorescence emission after pulse excitation with near-UV radiation. The phosphorescence signal was substantially (more than 50-fold) amplified by a covalently bound fluorescent dye (PromoFluor-555 or PromoFluor-647) whose absorption spectrum well overlapped with the phosphorescence emission spectrum of the selenium-containing heteroaromatic tricycle. The developed organic small-mol. long-lifetime photoluminescence probes possess subnanomolar affinity towards kinases of the PIM family and reveal especially strong emission signal with PIM-2 isoenzyme. The developed probes have potential to be used for monitoring of activity of PIM kinases for diagnosis of cancer. In the experiment, the researchers used many compounds, for example, Ethyl 3-amino-5-bromobenzofuran-2-carboxylate (cas: 330555-71-0Product Details of 330555-71-0).

Ethyl 3-amino-5-bromobenzofuran-2-carboxylate (cas: 330555-71-0) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antioxidant, antitubercular, antiplasmodial, insecticidal.Product Details of 330555-71-0

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Sequential targeting TGF-β signaling and KRAS mutation increases therapeutic efficacy in pancreatic cancer was written by Pei, Yuanyuan;Chen, Liang;Huang, Yukun;Wang, Jiahao;Feng, Jingxian;Xu, Minjun;Chen, Yu;Song, Qingxiang;Jiang, Gan;Gu, Xiao;Zhang, Qian;Gao, Xiaoling;Chen, Jun. And the article was included in Small in 2019.Safety of (3R,3aR)-3-(Furan-3-yl)-3a,7-dimethyl-3a,4,5,6-tetrahydroisobenzofuran-1(3H)-one This article mentions the following:

Pancreatic cancer is a highly aggressive malignancy that strongly resists extant treatments. The failure of existing therapies is majorly attributed to the tough tumor microenvironment (TME) limiting drug access and the undruggable targets of tumor cells. The formation of suppressive TME is regulated by transforming growth factor beta (TGF-β) signaling, while the poor response and short survival of almost 90% of pancreatic cancer patients results from the oncogenic KRAS mutation. Hence, simultaneously targeting both the TGF-β and KRAS pathways might dismantle the obstacles of pancreatic cancer therapy. Here, a novel sequential-targeting strategy is developed, in which antifibrotic fraxinellone-loaded CGKRK-modified nanoparticles (Frax-NP-CGKRK) are constructed to regulate TGF-β signaling and siRNA-loaded lipid-coated calcium phosphate (LCP) biomimetic nanoparticles (siKras-LCP-ApoE3) are applied to interfere with the oncogenic KRAS. Frax-NP-CGKRK successfully targets the tumor sites through the recognition of overexpressed heparan sulfate proteoglycan, reverses the activated cancer-associated fibroblasts (CAFs), attenuates the dense stroma barrier, and enhances tumor blood perfusion. Afterward, siKras-LCP-ApoE3 is efficiently internalized by the tumor cells through macropinocytosis and specifically silencing KRAS mutation. Compared with gemcitabine, this sequential-targeting strategy significantly elongates the lifespans of pancreatic tumor-bearing animals, hence providing a promising approach for pancreatic cancer therapy. In the experiment, the researchers used many compounds, for example, (3R,3aR)-3-(Furan-3-yl)-3a,7-dimethyl-3a,4,5,6-tetrahydroisobenzofuran-1(3H)-one (cas: 28808-62-0Safety of (3R,3aR)-3-(Furan-3-yl)-3a,7-dimethyl-3a,4,5,6-tetrahydroisobenzofuran-1(3H)-one).

(3R,3aR)-3-(Furan-3-yl)-3a,7-dimethyl-3a,4,5,6-tetrahydroisobenzofuran-1(3H)-one (cas: 28808-62-0) belongs to benzofurans derivatives. Benzofuran derivatives are one of the most important oxygen-containing heterocycles. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.Safety of (3R,3aR)-3-(Furan-3-yl)-3a,7-dimethyl-3a,4,5,6-tetrahydroisobenzofuran-1(3H)-one

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Pd-Catalyzed Synthesis of Aryl and Heteroaryl Triflones from Reactions of Sodium Triflinate with Aryl (Heteroaryl) Triflates was written by Smyth, Lynette A.;Phillips, Eric M.;Chan, Vincent S.;Napolitano, Jose G.;Henry, Rodger;Shekhar, Shashank. And the article was included in Journal of Organic Chemistry in 2016.Application In Synthesis of Benzofuran-5-ol This article mentions the following:

A novel method for Pd-catalyzed triflination of aryl and heteroaryl triflates using NaSO₂CF₃ as the nucleophile is described. The combination of Pd₂(dba)₃ and RockPhos formed the most effective catalyst. A broad range of functional groups and heteroaromatic compounds were tolerated under the neutral reaction conditions. The order of reactivity ArOTf ≥ ArCl ≥ ArBr is consistent with transmetalation being a slow step of the reaction. In the experiment, the researchers used many compounds, for example, Benzofuran-5-ol (cas: 13196-10-6Application In Synthesis of Benzofuran-5-ol).

Benzofuran-5-ol (cas: 13196-10-6) belongs to benzofurans derivatives. Benzofuran is the “”parent”” of many related compounds with more complex structures. For example, psoralen is a benzofuran derivative that occurs in several plants. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antioxidant, antitubercular, antiplasmodial, insecticidal.Application In Synthesis of Benzofuran-5-ol

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Effects of cationic and anionic micelles on the redox reaction of Erythrosine B by H₂O₂ in presence of Cu-Fe nanoparticles was written by Khan, Zaheer;AL-Thabaiti, Shaeel Ahmad;Singh, Bhawana;Rafiquee, M. Z. A.. And the article was included in International Journal of Chemical Kinetics.Reference of 16423-68-0 This article mentions the following:

Kinetic investigation of the degradation of Erythrosine B (EB) by H₂O₂ and copper-iron bimetallic nanoparticles was carried out spectrophotometrically. The degradation was carried out under the condition of sonication at 40°C. The co-precipitation method was used for the fabrication of CuO/Fe₂O₃ (Cu-Fe) in an alk. solution and characterized by SEM, XRD, FTIR, TEM, EDS, and BET methods. In the absence of the Cu-Fe, no degradation of EB by H₂O₂ was observed The presence of Cu-Fe resulted into the degradation of EB by H₂O₂. The kinetics of the degradation was studied under the conditions of variation of the amount of nanoparticles and at different concentrations of EB, H₂O₂, H⁺, surfactants (sodium dodecyl sulfate; SDS and cetyltrimethylammonium bromide; CTABr). The rate of reaction depends on the amount of Cu-Fe and [H₂O₂]. The rate constant values gave the peaked like curve (with maximum value at pH 3) at different pH. The dye degradation decreased with the increase in presence of (SDS) and (CTABr). In the experiment, the researchers used many compounds, for example, Sodium 2′,4′,5′,7′-tetraiodo-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-bis(olate) (cas: 16423-68-0Reference of 16423-68-0).

Sodium 2′,4′,5′,7′-tetraiodo-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-bis(olate) (cas: 16423-68-0) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.Reference of 16423-68-0

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Pharmacokinetics, Bioequivalence, and Safety Studies of Prucalopride in Healthy Chinese Subjects was written by Zhou, Ziye;Wang, Chenxiang;Zheng, Xuyong;Yu, Xuben;Yu, Chao;Zhang, Dongchuan;Xia, Yan;Chen, Huafang;Huang, Xiaoxiao;Zhang, Xiuhua. And the article was included in Clinical Pharmacology in Drug Development in 2020.Name: 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide This article mentions the following:

To evaluate the bioequivalence of 2 tablet formulations of prucalopride, generic and branded, and to investigate relevant pharmacokinetic and safety profiles. This study was designed as a randomized, open-label, fasting, single-dose, crossover, and dual-period trial. After overnight fasting, 12 subjects were given prucalopride tablets via oral administration, and blood specimens were obtained up to 96 h after dosing. Prucalopride concentrations in plasma were measured using ultraprecision liquid chromatog.-tandem mass spectrometry followed by calculation of pharmacokinetic parameters. The safety of prucalopride was assessed throughout the study. The pharmacokinetics of prucalopride can be defined as a 2-compartment model with a long elimination phase. No significant differences were observed between the pharmacokinetic profiles of the generic and branded prucalopride tablets. Bioequivalence was evaluated using 90%CIs for the ratio test/reference of log area under the concentration-time curve over 96 h, log area under the concentration-time curve to infinity, and log peak concentration from generic and branded tablets. During administration of the medication, there were 18 adverse events in 6 subjects in the test formulation group and 19 cases of adverse events in 6 subjects in the reference formulation group (P > .05). No severe adverse effects were detected. These results suggest that generic and branded prucalopride tablets are bioequivalent and show similar safety profiles. In the experiment, the researchers used many compounds, for example, 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide (cas: 179474-81-8Name: 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide).

4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide (cas: 179474-81-8) belongs to benzofurans derivatives. Benzofuran is the “”parent”” of many related compounds with more complex structures. For example, psoralen is a benzofuran derivative that occurs in several plants. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antiviral, antimicrobial, antitumor, anti-inflammatory.Name: 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Electromagnetic Mill Promoted Mechanochemical Solvent-Free Palladium-Catalyzed Borylation of Aryl Bromides was written by Liu, Yunxia;Li, Xin;Liu, Qing;Li, Xinjin;Liu, Hui. And the article was included in Organic Letters in 2022.Application of 519054-55-8 This article mentions the following:

The electromagnetic mill (EMM) promoted mechanochem. solvent-free Pd-catalyzed borylation of aryl bromides using low Pd catalyst loading (0.05-0.5 mol %) was realized. This protocol exhibits many advantages, such as broad substrate scope, good functional group tolerance, short reaction times, no addnl. heating, and practical gram-scale synthesis. This EMM system not only showed excellent prospects for industrial application but also unlocked broad areas of solvent-free solid-state metal-catalyzed syntheses. In the experiment, the researchers used many compounds, for example, 2-(Benzofuran-5-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (cas: 519054-55-8Application of 519054-55-8).

2-(Benzofuran-5-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (cas: 519054-55-8) belongs to benzofurans derivatives. Benzofuran derivatives have shown many biological activities, including antifungal and antimicrobial properties, and acting as antagonists of H3 receptors and angiotensin II. Substituted benzofurans find applications such as fluorescent sensors, oxidants, in drug discovery, and in another field of chemistry and agriculture.Application of 519054-55-8

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Gut microbiota alteration and modulation in hepatitis B virus-related fibrosis and complications: molecular mechanisms and therapeutic inventions was written by Li, Yao-Guang;Yu, Zu-Jiang;Li, Ang;Ren, Zhi-Gang. And the article was included in World Journal of Gastroenterology in 2022.Recommanded Product: 80621-81-4 This article mentions the following:

Hepatitis B virus (HBV) has posed a threat to public health, mainly resulting in liver damage. With long-term accumulation of extracellular matrix, patients with chronic hepatitis B are at high risk of developing into liver fibrosis and cirrhosis and even life-threatening hepatic carcinoma. The occurrence of complications such as spontaneous bacterial peritonitis and hepatic encephalopathy greatly increases disability and mortality. With deeper understanding of the bidirectional interaction between the liver and the gut (gut-liver axis), there is a growing consensus that the human health closely relates to the gut microbiota. Supported by animal and human studies, the gut microbiota alters as the HBV-related liver fibrosis initials and progresses, characterized as the decrease of the ratio between “good” and “potentially pathogenic” microbes. When the primary disease is controlled via antiviral treatment, the gut microbiota dysfunction tends to be improved. Conversely, the recovery of gut microbiota can promote the regression of liver fibrosis. Therapeutic strategies targeted on gut microbiota (rifaximin, probiotics, engineered probiotics and fecal microbiota transplantation) have been applied to animal models and patients, obtaining satisfactory results. In the experiment, the researchers used many compounds, for example, (2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)-25-(Acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]pyrido[1,2-a]benzimidazole-1,15(2H)-dione (cas: 80621-81-4Recommanded Product: 80621-81-4).

(2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)-25-(Acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]pyrido[1,2-a]benzimidazole-1,15(2H)-dione (cas: 80621-81-4) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Recommanded Product: 80621-81-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Donor-directed immunologic safety of COVID-19 vaccination in renal transplant recipients was written by Kueht, Michael;Kirk, Katie;Scott Lea, A.;Stevenson, Heather L.;Fair, Jeff;Kathleen Gamilla-Crudo, A.;Hussain, Syed;Mujtaba, Muhammad. And the article was included in Human Immunology in 2022.Application of 24280-93-1 This article mentions the following:

Infection risk and COVID-19 outcomes make SARS-CoV-2 vaccination essential for solid-organ transplant recipients. Reports of immune activation after vaccination causing graft failure raise concerns, but data are limited. Here, we document graft function, donor-derived-cell-free-DNA(dd-cfDNA), and donor-specific antibodies (DSA) in solid-organ renal transplant recipients after vaccination. Retrospective demographics, graft function, and immunol. parameters were collected in 96 renal transplant patients one month after their second vaccine dose. For-cause biopsies were performed based on clinician judgment. Similar proportions of subjects experienced increases (39.6%) and decreases (44.8%) in serum creatinine in the post-vaccination period, p = 0.56. Similar proportions of subjects experienced increases (23%) and decreases (25%) in serum ddcfDNA in the post-vaccination period, p = 0.87. Post-vaccination changes in serum creatinine and ddcfDNA (r(95) = -0.04, p = 0.71), serum creatinine and cumulative DSA MFI (r(95) = 0.07, p = 0.56), and ddcfDNA and cumulative DSA MFI (r(95) = 0.13, p = 0.21) were not significantly correlated. Five subjects had increased cumulative DSA MFI, but there were no de novo cases. Biopsies on three subjects confirmed pre-existing diagnoses. Our study found minimal evidence of donor-directed immunol. activity post-vaccination, and all immunol. changes did not correlate to graft dysfunction. We believe these findings do not amount to evidence of post-vaccination deleterious donor-directed activation. SARS-CoV-2 vaccination is immunol. safe and should continue for renal transplant recipients. In the experiment, the researchers used many compounds, for example, (E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enoic acid (cas: 24280-93-1Application of 24280-93-1).

(E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enoic acid (cas: 24280-93-1) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antiviral, antimicrobial, antitumor, anti-inflammatory.Application of 24280-93-1

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

A targeted library screen reveals a new inhibitor scaffold for protein kinase D was written by Tandon, Manuj;Wang, Lirong;Xu, Qi;Xie, Xiangqun;Wipf, Peter;Wang, Qiming Jane. And the article was included in PLoS One in 2012.Category: benzofurans This article mentions the following:

Protein kinase D (PKD) has emerged as a potential therapeutic target in multiple pathol. conditions, including cancer and heart diseases. Potent and selective small mol. inhibitors of PKD are valuable for dissecting PKD-mediated cellular signaling pathways and for therapeutic application. In this study, we evaluated a targeted library of 235 small organic kinase inhibitors for PKD1 inhibitory activity at a single concentration Twenty-eight PKD inhibitory chemotypes were identified and six exhibited excellent PKD1 selectivity. Five of the six lead structures share a common scaffold, with compound 139 being the most potent and selective for PKD vs PKC and CAMK. Compound 139 was an ATP-competitive PKD1 inhibitor with a low double-digit nanomolar potency and was also cell-active. Kinase profiling anal. identified this class of small mols. as pan-PKD inhibitors, confirmed their selectivity again PKC and CAMK, and demonstrated an overall favorable selectivity profile that could be further enhanced through structural modification. Furthermore, using a PKD homol. model based on similar protein kinase structures, docking modes for compound 139 were explored and compared to literature examples of PKD inhibition. Modeling of these compounds at the ATP-binding site of PKD was used to rationalize its high potency and provide the foundation for future further optimization. Accordingly, using biochem. screening of a small number of privileged scaffolds and computational modeling, we have identified a new core structure for highly potent PKD inhibition with promising selectivity against closely related kinases. These lead structures represent an excellent starting point for the further optimization and the design of selective and therapeutically effective small mol. inhibitors of PKD. In the experiment, the researchers used many compounds, for example, 7-Hydroxy-2,3,4,5-tetrahydro-1H-benzofuro[2,3-c]azepin-1-one (cas: 521937-07-5Category: benzofurans).

7-Hydroxy-2,3,4,5-tetrahydro-1H-benzofuro[2,3-c]azepin-1-one (cas: 521937-07-5) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Category: benzofurans

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem